专利号:US-7034154-B2 优先权日:1999-08-10 标 题:Synthesis of substituted pyrazolopyrimidines 发明人:GROSS RAYMOND S; WILCOXEN KEITH M; OGLESBY RICHARD CHRISTOPHER 权利人:NEUROCRINE BIOSCIENCES INC 摘要:Methods of making substituted pyrazolopyrimidines generally and, more particularly, N-methyl-N-(3-{3-[2-thienylcarbonyl]-pyrazol-[1,5-α]-pyrimidin-7-yl}phenyl)acetamide. Such compounds have utility over a wide range of indications, including treatment of insomnia. In the practice of the present invention, improved techniques which do not require use and/or isolation of the pyrazole intermediate are disclosed, as well as improved techniques for making the reaction intermediates themselves. Such techniques offer significant advantages, including enhanced efficiency, particularly in the context of large scale manufacture.
专利号:US-7034163-B2 优先权日:2003-09-05 标 题 :Synthesis of pyrroles 发明人:PAGENKOPF BRIAN L; YU MING 权利人:UNIV TEXAS 摘要:An improved and highly efficient method for the preparation of 2-R(R=alkyl, aryl, H) pyrroles from nitrites (RCN, R=alkyl, aryl) is described using Lewis acid activated donor-acceptor cyclopropanes to react with aliphatic, aromatic, branched, α,β-unsaturated, or otherwise functionalized nitrites in a cascade [3+2] dipolar cycloaddition, dehydration and tautomerization sequence.
专利号:US-7094906-B2 优先权日:1998-04-20 标 题:Processes for preparing pesticidal intermediates 发明人:ANCEL JEAN-ERICK 权利人:BASF AGRO BV 摘要:The present invention relates to processes for the preparation of a compound of the formula n nwherein W is nitrogen or —CR 3 ; R 1 is halogen, haloalkyl, haloalkoxy, R 4 S(O) n — or —SF 5 ; R 2 is hydrogen or halogen; R 3 is halogen; R 4 is alkyl or haloalkyl; and n is 0, 1 or 2; and processes for using a compound of the formula (I) in the synthesis of compounds of the formula
专利号:JP-2003506453-A 优先权日:1999-08-10 标题 :Synthesis of substituted pyrazolopyrimidines
专利号:EP-3929197-B1 优先权日:2015-08-12 标 题:Intermediates for the synthesis of microbiocidal heterobicyclic derivatives
专利号:US-2005054857-A1 优先权日:2003-09-05 标 题:Synthesis of pyrroles